Lecture 13: Respiratory pharmacology Flashcards
What are the three categories of bronchodilator?
Adrenergic agonists - beta2 agonists (Salbutamol, Salmeterol, formoterol)
Anticholinergics (Tiotropium, ipratropium)
Methylxanthines (Aminophylline)
What are the two categories of anti-inflammatory drug?
Steroids (Prednisolone, Beclomethasone) Leukotriene Inhibitors (Monteleukast)
What is the duration of action of salbutamol?
Short acting (begin immediately, 3-5 hour duration)
What is/are the routes of administration of salbutamol?
Inhaled or nebuliser (higher dose)
IV – very rarely used
What is the mechanism of action of salbutamol?
Binding to beta2 receptors in the lungs
Results in relaxation of bronchial smooth muscles
Increases cAMP production by activating adenylate cyclase and cAMP
What kind of drug is salbutamol?
SABA
Bronchodilator
What is salbutamol used for?
Asthma and COPD
Which drugs can be used in a medical emergency?
Salbutamol Tiotropium Ipratropium Theophylline Oxygen
What is the duration of salmeterol?
Long acting (begin 2-30 min, 10-12 hour dur)
What is the route of salmeterol administration?
Inhaled
What kind of drug is salmeterol?
LABA
Bronchodilator
What is salmeterol used for?
Asthma: in patients requiring long-term regular bronchodilator therapy on ICS
(always used with ICS in asthma)
COPD: persistent symptoms despite therapy
(either stand alone or as ICS/LABA combination FEV1 < 50%)
What is the duration of formoterol?
Long acting (with short onset similar to salbutamol but with prolonged duration 10-12 hours)
What is the route of formoterol administration?
Inhaled
What type of drug is formoterol?
LABA
Bronchodilator
What is formoterol used for?
Asthma
(always combined with ICS)
MART
COPD
What is the duration of tiotropium?
Long acting (24 hour) – one a day
What is the route of tiotropium administration?
Inhaled (Dry powder Handihaler/Mist resimat)
What is tiotropiums mechanism of action?
Similar affinity to the subtypes of muscarinic receptors, M1 to M5
In the airways, it exhibits pharmacological effects through inhibition of M3-receptors at the smooth muscle leading to bronchodilatation
What type of drug is tiotropium?
LAMA
Anticholinergic
Bronchodilator
When is tiotropium used?
Stable COPD: Symptoms despite SABA (any severity and with LABA)
Asthma: in not improving despite ICS/LABA specialist treatment from hospital
What type of drug is ipratropium?
SAMA
Anticholinergic
Bronchodilator
What is the duration of ipratropium?
Onset 30 minutes; lasts 6 hours
What is the method of administration of ipratropium?
MDI
Nebulised
When is ipratropium used?
Nebulised for acute presentations of COPD and sometimes asthma
What is the duration of theophylline action?
Half life around 5 hours healthy adults
What is the route of theophylline administration?
Oral
IV
What is the mechanism of theophylline action?
Phosphodiesterase inhibitor
Requires monitoring of level (blood test)
When is theophylline used?
PO: COPD and asthma –persistent symptoms
IV: COPD and asthma medical emergencies
What are the adverse events of the bronchodilators?
Tachycardia
Nervousness
Irritability
Tremor
Inhaled preparations: less common
Oral preparations (hardly used): More common Tachyarrhythmias Angina
Usually dose related
Which glucocorticoid is systemic?
Prednisolone
What are the features of systemic glucocorticoids?
IV or oral
Stronger effects
Action unaffected by lung restriction
More side effects, esp with long term therapy
Which glucocorticoid is inhaled?
Beclometasone
What are the key features of inhaled glucocorticoids?
Localized action
Fewer side effects: some absorption occurs
Disease may prevent penetration of drug to affected areas
What are the airway effects of glucocorticoids?
Decrease release of inflammatory mediator
Decrease infiltration and action of WBCs
Decrease airway oedema
Decrease airway mucus production
Increase number and sensitivity of beta-2 receptors
What are the possible side effects of glucocorticoids?
Oral candidiasis
Dysphonia
Adrenal suppression
Bone loss
Slow growth in children, but not ultimate height
Increase risk of cataracts and glaucoma
Increased risk of infection
Gastric ulceration
Hypertension
Diabetes
Mood disturbance
What are antihistamines?
Allergic rhinitis medications
Cetirizine, Chlorpheniramine
H1 antagonists
Side effects: Drowsiness, Dry Mouth, Dry Eyes, Confusion
What are intranasal glucocorticoids used for?
Allergic rhinitis medication
What is monteleukast?
Allergic rhinitis medication
Inhibit leukotriene receptors
↓inflammation, bronchoconstriction, oedema, mucus, recruitment of eosinophils
What are sympathomimetics?
Allergic rhinitis medication
Decongestants
What is amoxicillin?
Penicillin
Moderate-spectrum, bacteriolytic, B lactam antibiotic
What is amoxicillins routes of administration?
IV
Oral
When is amoxicillin used?
CAP
COPD exacerbations
Bronchitis
What type of bacteria is killed by amoxicillin?
Gram negative and gram positive
What is co-amoxiclav?
Penicillin
Amoxicillin is susceptible to degradation by B lactamase -producing bacteria so can be combined with clavulinic acid – a beta lactamase inhibitor
What are tetracyclines?
Antibiotics
Tetracycline inhibits protein synthesis
Broad spectrum action Gram positive and negative
Useful for ‘atypical infections’ e.g. mycoplasma, legionella
Name a tetracycline.
Doxycycline
What is the route of tetracycline administration?
Oral
What are the side effects of tetracyclines?
GI Upset Staining teeth Lupus Allergy Photosensitivity
What are quiolones?
Antibiotic
Mechanism of action - DNA fragmentation
Name a quinolone.
Ciprofloxacin
Moxifloxacin
What is the route of administration of quinolones?
IV
Oral
Inhaled (CF)
What are the side effects of quinolones?
GI upset C difficile Tendonitis Liver upset Prolonged QTc and arrthymia
What are macrolides?
Antibiotics
Mechanism of action - Protein synthesis inhibitors
Name a macrolide.
Erythromycin
Clarithromycin
What is the route of macrolide administration?
IV
Oral
What bacteria are killed by quinolones?
Gram negative and positive coverage (And Pseudomonas)
What bacteria are killed by macrolides?
Gram positive /limited gram negative cover
What are the side effects of macrolides?
GI
Allergy
Liver abnormality
Prolonged QTc and interactions
What can be used to treat some idiopathic interstitial pneumonias (hypersensitivity pneumonia)?
Prednisolone
Azathioprine
MMF
What can be used to treat sarcoid?
Prednisolone
What can be used to treat idiopathic pulmonary fibrosis?
Pirfenidone
Anti inflammatory/ Anti Fibrotic
Reduces fibroblast proliferation
Reduces collagen production
